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researcher

Richard Wheelhouse

Reader in Medicinal Chemistry

Faculty/Dept/School School of Pharmacy and Medical Sciences
(Faculty of Life Sciences)
Emailr.t.wheelhouse@bradford.ac.uk
Telephone +441274 234710

Biography

2017–     Associate Head, Internationalisation, School of Pharmacy and Medical Sciences, 
2016–     Honorary Professor, Faculty of Pharmacy, University of Khartoum, Sudan
2014–     Reader in Medicinal Chemistry, 
2006–     EPSRC Peer Review College, nominated by the community.

Research

  • Medicinal Chemistry 
  • Biophysics 
  • Anticancer Drugs 
  • Drug-Nucleic Acid Interactions 
  • Imidazotetrazines 
  • NMR
  • UV 
Date Role Title / Description Funder Award
- PIImidazotetrazine Prodrugs
- PITargeting DNA·RNA Hybrid Duplexes

Professional activities

  • 01-APR-09: Brown Cancer Center, University of Louisville, Kentucky, USA - Visiting Research Scientist
  • 01-JAN-06: Bradford School of Pharmacy - Head, Division of Pharmaceutics and Pharmaceutical Chemistry
  • 01-MAR-98: Bradford School of Pharmacy - Lecturer
  • 01-JAN-96: The University of Texas at Austin, USA - Research Fellow
  • 01-JAN-92: The University of Nottingham, UK - Senior Research Fellow
  • 01-JAN-90: Aston University,  Birmingham, UK - Research Associate
  • Editorial Board Member (Chemistry) Scientific Reports, Nature Publishing ,
  • 01-JAN-06: EPSRC Peer Review College,
  • CChem FRSC
  • member
  • 01-OCT-09: WO2009127815 - Aminoalkyl Imidazotetrazines for Treatment of Cancer
  • 01-JAN-98: WO 98/33503 - Porphyrin Compounds as Telomerase Inhibitors

Publications

Peer Reviewed Journal
TitleRuthenium-Containing Linear Helicates and Mesocates with Tuneable p53-Selective Cytotoxicity in Colorectal Cancer Cells. (2018)
AuthorsAllison SJ;Cooke D;Davidson FS;Elliott PIP;Faulkner RA;Griffiths HBS;Harper OJ;Hussain O;Owen-Lynch PJ;Phillips RM;Rice CR;Shepherd SL;Wheelhouse RT;
JournalAngewandte Chemie - International Edition
DOI10.1002/anie.201805510
 
TitleSynthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position (2018)
AuthorsDavid Cousin;Marc G. Hummersone;Tracey D. Bradshaw;Jihong Zhang;Christopher J. Moody;Magdalena B. Foreiter;Helen S. Summers;William Lewis;Richard T. Wheelhouse;Malcolm F. G. Stevens;
JournalMedChemComm
DOI10.1039/c7md00554g
 
TitleEvaluation of Novel Imidazotetrazine Analogues Designed to Overcome Temozolomide Resistance and Glioblastoma Regrowth (2015)
AuthorsRamirez, Y.P.; Mladek, A.C.; Phillips, Roger M.; Gynther, M.; Rautio, J.; Ross, A.H.; Wheelhouse, Richard T.; Sakaria, J.N.
 
TitleStabilization of a bimolecular triplex by 3'-S-phosphorothiolate modifications: An NMR and UV thermal melting investigation (2015)
AuthorsEvans, K.;Bhamra, I.;Wheelhouse, R.T.;Arnold, J.R.P.;Cosstick, R.;Fisher, J.;
JournalCHEMISTRY - A EUROPEAN JOURNAL
DOI10.1002/chem.201500369
 
TitleThe medicinal chemistry of imidazotetrazine prodrugs (2014)
AuthorsMoody, C.L.;Wheelhouse, R.T.;
JournalPharmaceuticals
DOI10.3390/ph7070797
 
TitleSynthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA- methyltransferase, DNA mismatch repair, and p53 (2013)
AuthorsPletsas, D.;Garelnabi, E.A.E.;Li, L.;Phillips, R.M.;Wheelhouse, R.T.;
JournalJournal of Medicinal Chemistry
DOI10.1021/jm401121k
 
TitleGlioblastoma multiforme therapy and mechanisms of resistance (2013)
AuthorsRamirez Y.;Weatherbee J.;Wheelhouse R.;Ross A.
JournalPharmaceuticals
DOI10.3390/ph6121475
 
TitleMetabolism of cryptolepine and 2-fluorocryptolepine by aldehyde oxidase (2012)
AuthorsStell, J.G.P.;Wheelhouse, R.T.;Wright, C.W.;
JournalJournal of Pharmacy and Pharmacology
DOI10.1111/j.2042-7158.2011.01408.x
 
TitleStrategy for imidazotetrazine prodrugs with anticancer activity independent of MGMT and MMR (2012)
AuthorsGarelnabi, E.A.E.;Pletsas, D.;Li, L.;Kiakos, K.;Karodia, N.;Hartley, J.A.;Phillips, R.M.;Wheelhouse, R.T.;
JournalACS Medicinal Chemistry Letters
DOI10.1021/ml300132t
 
TitleMinor structural modifications to alchemix influence mechanism of action and pharmacological activity (2012)
AuthorsAbdallah Q.;Phillips R.;Johansson F.;Helleday T.;Cosentino L.;Abdel-Rahman H.;Etzad J.;Wheelhouse R.;Kiakos K.;Bingham J.;Hartley J.;Patterson L.;Pors K.
JournalBiochemical Pharmacology
DOI10.1016/j.bcp.2012.02.017
 
TitleProbing the molecular recognition of a DNA·RNA hybrid duplex (2010)
AuthorsWheelhouse R.;Garbett N.;Buurma N.;Chaires J.
JournalAngewandte Chemie - International Edition
DOI10.1002/anie.200907235
 
TitlePolar, Functionalized Guanine-O6 Derivatives Resistant to Repair by O6-Alkylguanine-DNA Alkyltransferase: Implications for the Design of DNA-modifying Drugs. (2009)
AuthorsWheelhouse, Richard T.; Bibby, Michael C.; Nicolaou, Anna; Pletsas, Dimitrios
 
TitleA cytotoxic diterpenoid from Croton membranaceus, the major constituent of anticancer herbal formulations used in Ghana (2008)
AuthorsBayor, M.T.;Ayim, J.S.K.;Marston, G.;Phillips, R.M.;Shnyder, S.D.;Wheelhouse, R.T.;Wright, C.W.;
JournalNatural product communications
 
TitleA safe, convenient and efficient method for the preparation of heterocyclic N-oxides using urea·hydrogen peroxide (2008)
AuthorsRong D.;Phillips V.;Rubio R.;Ángeles Castro M.;Wheelhouse R.
JournalTetrahedron Letters
DOI10.1016/j.tetlet.2008.09.124
 
TitleInhibition of cobalamin-dependent methionine synthase by substituted benzo-fused heterocycles (2007)
AuthorsBanks E.;Doughty S.;Toms S.;Wheelhouse R.;Nicolaou A.
JournalFEBS Journal
DOI10.1111/j.1742-4658.2006.05583.x
 
TitlePolar, functionalized guanine-O6 derivatives resistant to repair by O6-alkylguanine-DNA alkyltransferase: implications for the design of DNA-modifying drugs (2006)
AuthorsPletsas D.;Wheelhouse R.;Pletsa V.;Nicolaou A.;Jenkins T.;Bibby M.;Kyrtopoulos S.
JournalEuropean Journal of Medicinal Chemistry
DOI10.1016/j.ejmech.2005.11.007
 
TitleDesign, synthesis, and evaluation of novel biarylpyrimidines: A new class of ligand for unusual nucleic acid structures (2006)
AuthorsWheelhouse R.;Jennings S.;Phillips V.;Pletsas D.;Murphy P.;Garbett N.;Chaires J.;Jenkins T.
JournalJournal of Medicinal Chemistry
DOI10.1021/jm060315a
 
TitleIn-vitro cytotoxic activities of the major bromophenols of the red alga Polysiphonia lanosa and some novel synthetic isomers (2004)
AuthorsShoeib N.;Bibby M.;Blunden G.;Linley P.;Swaine D.;Wheelhouse R.;Wright C.
JournalJournal of Natural Products
DOI10.1021/np0305268
 
TitleBiarylpyrimidines: a new class of ligand for high-order DNA recognition. (2003)
AuthorsMurphy PM;Phillips VA;Jennings SA;Garbett NC;Chaires JB;Jenkins TC;Wheelhouse RT;
JournalCHEMICAL COMMUNICATIONS (PRINT)
DOI10.1039/b301554h
 
TitleA novel, high-yielding synthesis of meso-substituted porphyrins via the direct arylation of porphine (2002)
AuthorsShi D.;Wheelhouse R.
JournalTetrahedron Letters
DOI10.1016/S0040-4039(02)02339-0
 
TitleA 15N NMR investigation of a series of benzotriazinones and related antitumour heterocycles (2002)
AuthorsVaughan, K.;Wilman, D.E.V.;Wheelhouse, R.T.;Stevens, M.F.G.;
JournalMagnetic Resonance in Chemistry
DOI10.1002/mrc.994
 
TitleQuadruplex-interactive agents as telomerase inhibitors: Synthesis of porphyrins and structure-activity relationship for the inhibition of telomerase (2001)
AuthorsShi D.;Wheelhouse R.;Sun D.;Hurley L.
JournalJournal of Medicinal Chemistry
DOI10.1021/jm010246u
 
TitleAntitumour imidazotetrazines. Part 39. Synthesis of bis(imidazotetrazine)s with saturated spacer groups (2000)
AuthorsArrowsmith J.;Jennings S.;Langnel D.;Wheelhouse R.;Stevens M.
JournalJournal of the Chemical Society, Perkin Transactions 1
DOI10.1039/b005652i
 
TitleG-quadruplexes as targets for drug design (2000)
AuthorsHurley, L.H.;Wheelhouse, R.T.;Sun, D.;Kerwin, S.M.;Salazar, M.;Fedoroff, O.Y.;Han, F.X.;Han, H.;Izbicka, E.;Von Hoff, D.D.;
JournalPharmacology and Therapeutics
DOI10.1016/S0163-7258(99)00068-6
 
TitleTelomere-interactive agents affect proliferation rates and induce chromosomal destabilization in sea urchin embryos (1999)
AuthorsIzbicka E.;Nishioka D.;Marcell V.;Raymond E.;Davidson K.;Lawrence R.;Wheelhouse R.;Hurley L.;Wu R.;Von Hoff D.
JournalAnti-Cancer Drug Design
 
TitleEffects of cationic porphyrins as G-quadruplex interactive agents in human tumor cells (1999)
AuthorsIzbicka E.;Wheelhouse R.;Raymond E.;Davidson K.;Lawrence R.;Sun D.;Windle B.;Hurley L.;Von Hoff D.
JournalCancer Research
 
TitleInteractions of TMPyP4 and TMPyP2 with quadruplex DNA. Structural basis for the differential effects on telomerase inhibition (1999)
AuthorsHan, F.X.;Wheelhouse, R.T.;Hurley, L.H.;
JournalJournal of the American Chemical Society
DOI10.1021/ja984153m
 
TitleCationic porphyrins as telomerase inhibitors: The interaction of tetra- (N-methyl-4-pyridyl)porphine with quadruplex DNA [1] (1998)
AuthorsWheelhouse, R.T.;Sun, D.;Han, H.;Han, F.X.;Hurley, L.H.;
JournalJournal of the American Chemical Society
DOI10.1021/ja973792e
 
TitleMechanism for the catalytic activation of ecteinascidin 743 and its subsequent alkylation of guanine N2 (1998)
AuthorsMoore II, B.M.;Seaman, F.C.;Wheelhouse, R.T.;Hurley, L.H.;
JournalJournal of the American Chemical Society
DOI10.1021/ja974109r
 
TitleAntitumour imidazotetrazines. Part 36. Conversion of 5-aminoimidazole-4-carboxamide to imidazo[5,1-d][1,2,3,5]tetrazin-4(3H)-ones and imidazo[1,5-a][1,3,5]triazin-4(3H)-ones related in structure to the antitumour agents temozolomide and mitozolomide (1998)
AuthorsWang, Y.;Wheelhouse, R.T.;Zhao, L.;Langnel, D.A.F.;Stevens, M.F.G.;
JournalJournal of the Chemical Society, Perkin Transactions 1
 
TitleTemozolomide: A review of its discovery, chemical properties, pre-clinical development and clinical trials (1997)
AuthorsNewlands, E.S.;Stevens, M.F.G.;Wedge, S.R.;Wheelhouse, R.T.;Brock, C.;
JournalCancer Treatment Reviews
DOI10.1016/S0305-7372(97)90019-0
 
TitleAntitumour benzothiazoles. Part 4. An NMR study of the sites of protonation of 2-(4-aminophenyl)benzothiazoles (1996)
AuthorsWheelhouse, R.T.;Shi, D.-F.;Wilman, D.E.V.;Stevens, M.F.G.;
JournalJournal of the Chemical Society, Perkin Transactions 2
 
TitleAntitumour imidazotetrazines. Part 31. The synthesis of isotopically labelled temozolomide and a multinuclear (1H, 13C, 15N) magnetic resonance investigation of temozolomide and mitozolomide (1995)
AuthorsR.T. Wheelhouse,* D.E.V. Wilman, W. Thomson, M.F.G. Stevens
JournalJournal of the Chemical Society, Perkin Transactions 1
 
TitleStructural studies on bioactive compounds. Part 27. Chemistry of the immunomodulatory agent bropirimine. (1995)
AuthorsStevens MF;Baig GU;Gate EN;Wheelhouse RT;
JournalAnti-Cancer Drug Design
 
TitleAntitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide. (1995)
AuthorsClark AS;Deans B;Stevens MF;Tisdale MJ;Wheelhouse RT;Denny BJ;Hartley JA;
JournalMedicinal Chemistry
DOI10.1021/jm00009a010
 
TitleNMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA. (1994)
AuthorsDenny BJ;Wheelhouse RT;Stevens MF;Tsang LL;Slack JA;
JournalJournal of Biochemistry
DOI10.1021/bi00197a003
 
TitleDecomposition of the antitumour drug temozolomide in deuteriated phosphate buffer: Methyl group transfer is accompanied by deuterium exchange (1993)
AuthorsWheelhouse, R.T.;Stevens, M.F.G.;
JournalJournal of the Chemical Society - Series Chemical Communications
 
TitleTargeting of cytotoxic agents by polyamines: Synthesis of a chlorambucil-spermidine conjugate (1992)
AuthorsCohen, G.M.;Cullis, P.M.;Hartley, J.A.;Mather, A.;Symons, M.C.R.;Wheelhouse, R.T.;
JournalChemical Communications
 
TitleTargeting of tumor cells and DNA by a chlorambucil-spermidine conjugate. (1992)
AuthorsHolley JL;Mather A;Wheelhouse RT;Cullis PM;Hartley JA;Bingham JP;Cohen GM;
JournalCancer Research
 
TitleMotion of polyammonium ions on aqueous solutions of DNA (1990)
AuthorsBesley, S.;Cullis, P.M.;Partridge, R.;Symons, M.C.R.;Wheelhouse, R.T.;
JournalChemical Physics Letters
DOI10.1016/0009-2614(90)85415-9
 
Book Chapter
TitleHeterocyclic N-oxidation Using Urea-Hydrogen Peroxide: a Safe, Convenient and Effective source of Hydrogen Peroxide. (2009)
AuthorsD. Rong, V.A. Phillips, R.T. Wheelhouse.
JournalCurrent Issues in Organic Chemistry
PublisherHeron Press
 
TitleNMR and Molecular Modelling Studies on the Mechanism of Action of the Antitumour Drug Temozolomide. (1995)
AuthorsR.T. Wheelhouse,* B.J. Denny, M.F.G. Stevens
JournalContributions to Oncology 49: Novel Approaches in Anticancer Drug Design
PublisherS. Karger
 
Other Publication
Other typeReviews
TitleThe medicinal chemistry of imidazotetrazine prodrugs (2014)
AuthorsMoody C.;Wheelhouse R.
JournalPharmaceuticals
DOI10.3390/ph7070797